pd 153035 analog 30

Lifirafenib, also known as Beigene-283, is a Novel potent and selective RAF Kinase and EGFR inhibitor. BGB-283-displays Potent Antitumor Activity in B-RAF Mutated Colorectal Cancers. In vitro, BGB-283 potently inhibits B-RAFV600E-activated ERK phosphorylation and cell proliferation. It demonstrates selective cytotoxicity and preferentially inhibits proliferation of cancer cells harbouring B-RAFV600E and EGFR mutation amplification. In B-RAFV600E CRC cell lines, BGB-283 effectively inhibits the reactivation of EGFR and EGFR-mediated cell proliferation. In vivo, BGB-283 treatment leads to dose-dependent tumor growth inhibition accompanied by partial and complete tumor regressions in both cell-line derived and primary human colorectal tumor xenografts bearing B-RAFV600E mutation. BGB-283 as a potent antitumor drug candidate with clinical potential for treating CRC harbouring B-RAFV600E mutation.

Lifirafenib (Beigene-283) 是新型高效的Raf 激酶和EGFR 抑制剂，对重组BRafV600E 和EGFR 的IC50值分别为 23 和 29 nM。